Powder: -20°C for 3 years | In solvent: -80°C for 1 year
hMAO-B-IN-2 (compound 6j) 是具有口服活性、选择性的、且竞争性可逆的 hMAO-B 抑制剂 (IC 50 = 4 nM),可穿透血脑屏障。hMAO-B-IN-2 对 SH-SY5Y 细胞显示出良好的神经保护作用和低毒性,可用于阿尔茨海默症的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible inhibitor of hMAO-B (IC 50 = 4 nM) that can be used for the research of alzheimer’s disease. hMAO-B-IN-2 exhibits good neuroprotective effects and low toxicity in SH-SY5Y cell [1]. |
体外活性 | hMAO-B-IN-2 (compound 6j) (0-100 μM, 15 min) exhibits potent inhibitory activity, with IC 50 values of 4 nM (hMAO-B) and 6.04 nM (hMAO-A), respectively [1]. hMAO-B-IN-2 (30 min) is a reversible MAO-B inhibitor, the activity of MAO-B enzyme was restored to about 82% and 45% after compound 6j dilution to 0.1 × IC 50 and 1 × 50, respectively [1]. hMAO-B-IN-2 (25 μM, 48 h) exhibits remarkable inhibitory activities against MAO-B, had good inhibition property of Aβ self-induce aggregation (40.78 ± 6.27%) [1]. hMAO-B-IN-2 (0-100 μM, 24 h) shows non-toxic at the concentrations of 25 μM [1]. hMAO-B-IN-2 (0-25 μM, 24 h) has neuroprotective capability against neurodegeneration disease, and increases cell survival rates in a dose-dependent manner [1]. Cell Cytotoxicity Assay Cell Line: SH-SY5Y neuroblastoma cell [1] Concentration: 0, 6.25, 12.5, 25, 50, 100 μM Incubation Time: 24 h Result: Showed non-toxic at the concentrations of 25 μM. |
体内活性 | hMAO-B-IN-2 (compound 6j) (Sprague-Dawley rats; 3 mg/kg, IV; 10 mg/kg, PO; once) has acceptable pharmacokinetic properties [1]. Pharmacokinetic Parameters of hMAO-B-IN-2 in male Sprague-Dawley rats [1]. Parameters IV (3 mg/kg) PO (10 mg/kg) T 1/2 (h) 1.02 ± 0.17 1.33 ± 0.16 T max (h) 0.3 C max (μg/L) 639.29 ± 89.06 142.17 ± 72.21 AUC 0-inf (μg/L h) 247.74 ± 11.48 268.49 ± 69.72 CL (L/h/kg) 3.33 ± 0.15 F (%) 36.10% Animal Model: Sprague-Dawley rats (male, 220±20 g) [1] Dosage: 3 mg/kg (IV), 10 mg/kg (PO) Administration: IV, PO (Pharmacokinetic Analysis) Result: Had acceptable pharmacokinetic properties, and showed a high maximal concentration, appropriate half-life, and good oral bioavailability. |
分子量 | 301.38 |
分子式 | C18H23NO3 |
CAS No. | 2454459-87-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
hMAO-B-IN-2 2454459-87-9 Inhibitor inhibitor inhibit